کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371788 | 981856 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
γ-Carbolines: A novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: γ-Carbolines: A novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration γ-Carbolines: A novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration](/preview/png/1371788.png)
چکیده انگلیسی
An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. γ-Carbolines are a novel class of potent mixed CB1/CB2 agonists characterized by attractive physicochemical properties including high aqueous solubility. Optimization of the series has led to the discovery of 29, which has oral activity in a rat inflammatory pain model and limited brain exposure at analgesic doses, consistent with a lower risk of CNS-mediated tolerability issues.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 4, 15 February 2012, Pages 1619–1624
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 4, 15 February 2012, Pages 1619–1624
نویسندگان
Yun-Xing Cheng, Mehrnaz Pourashraf, Xuehong Luo, Sanjay Srivastava, Christopher Walpole, Dominic Salois, Stephane St-Onge, Kemal Payza, Etienne Lessard, Xiao Hong Yu, Mirosław J. Tomaszewski,